Intermediates of duocarmycin sa and its derivatives and...

Details Intermediates of duocarmycin sa and its derivatives and... Intermediates of duocarmycin sa and its derivatives and...

C - Chemistry, Metallurgy

07

D

C07D 487/04 (2006.01) A61K 31/40 (2006.01) C07D 209/12 (2006.01)

Patent

CA 2266505

Indole derivatives of general formulae (1), (2a) and (2b) and pyrroloindole derivatives of general formula (3) useful as intermediates for the preparation of duocarmycin SA and derivatives thereof which are expected to be useful as anticancer drugs; and a process for the preparation of these derivatives, wherein R1 is an amino-protecting group; R2 is a hydroxyl-protecting group; R3 is a hydroxyl-protecting group; and R4 is C1-C6 linear or branched lower alkyl or benzyl.

Cette invention concerne des dérivés d'indole correspondant aux formules générales (1), (2a) et (2b) où R?1¿ représente un groupe protecteur d'amino, R?2¿ et R?3¿ représentent chacun un groupe protecteur d'hydroxyle, et R?4¿ représente un benzyle ou alkyle inférieur C¿1?-C¿6? réticulé ou linéaire. Cette invention concerne également des dérivés de pyrroloindole correspondant à la formule générale (3). Ces dérivés sont utiles en qualité de produits intermédiaires dans la préparation de duocarmycine SA et de dérivés de ce dernier, lesquels peuvent être utilisés comme médicaments contre le cancer. Cette invention concerne enfin un procédé de préparation de ces dérivés.

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